Positron emitter labeled enzyme inhibitors
Abstract
This invention involved a new strategy for imaging and mapping enzyme activity in the living human and animal body using positron emitter-labeled suicide enzyme inactivators or inhibitors which become covalently bound to the enzyme as a result of enzymatic catalysis. Two such suicide in activators for monoamine oxidase have been labeled with carbon-11 and used to map the enzyme subtypes in the living human and animal body using PET. By using positron emission tomography to image the distribution of radioactivity produced by the body penetrating radiation emitted by carbon-11, a map of functionally active monoamine oxidase activity is obtained. Clorgyline and L-deprenyl are suicide enzyme inhibitors and irreversibly inhibit monoamine oxidase. When these inhibitors are labeled with carbon-11 they provide selective probes for monoamine oxidase localization and reactivity in vivo using positron emission tomography. 2 figs.
- Inventors:
- Issue Date:
- Research Org.:
- Brookhaven National Laboratory (BNL), Upton, NY (United States)
- OSTI Identifier:
- 6864415
- Patent Number(s):
- 6052921
- Assignee:
- TIC; EDB-88-179699
- Patent Classifications (CPCs):
-
A - HUMAN NECESSITIES A43 - FOOTWEAR A43C - FASTENINGS OR ATTACHMENTS OF FOOTWEAR
- DOE Contract Number:
- AC02-76CH00016
- Resource Type:
- Patent
- Resource Relation:
- Other Information: Portions of this document are illegible in microfiche products
- Country of Publication:
- United States
- Language:
- English
- Subject:
- 59 BASIC BIOLOGICAL SCIENCES; AMINE OXIDASES; ENZYME INHIBITORS; ENZYME ACTIVITY; DISTRIBUTION; LABELLING; CARBON 11; CHEMICAL PREPARATION; INVENTIONS; ORGANIC COMPOUNDS; POSITRON COMPUTED TOMOGRAPHY; BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; CARBON ISOTOPES; COMPUTERIZED TOMOGRAPHY; DIAGNOSTIC TECHNIQUES; EMISSION COMPUTED TOMOGRAPHY; ENZYMES; EVEN-ODD NUCLEI; ISOTOPES; LIGHT NUCLEI; MINUTES LIVING RADIOISOTOPES; NUCLEI; OXIDOREDUCTASES; RADIOISOTOPES; SYNTHESIS; TOMOGRAPHY; 550201* - Biochemistry- Tracer Techniques; 550200 - Biochemistry
Citation Formats
Fowler, J S, MacGregor, R R, and Wolf, A P. Positron emitter labeled enzyme inhibitors. United States: N. p., 1987.
Web.
Fowler, J S, MacGregor, R R, & Wolf, A P. Positron emitter labeled enzyme inhibitors. United States.
Fowler, J S, MacGregor, R R, and Wolf, A P. Fri .
"Positron emitter labeled enzyme inhibitors". United States.
@article{osti_6864415,
title = {Positron emitter labeled enzyme inhibitors},
author = {Fowler, J S and MacGregor, R R and Wolf, A P},
abstractNote = {This invention involved a new strategy for imaging and mapping enzyme activity in the living human and animal body using positron emitter-labeled suicide enzyme inactivators or inhibitors which become covalently bound to the enzyme as a result of enzymatic catalysis. Two such suicide in activators for monoamine oxidase have been labeled with carbon-11 and used to map the enzyme subtypes in the living human and animal body using PET. By using positron emission tomography to image the distribution of radioactivity produced by the body penetrating radiation emitted by carbon-11, a map of functionally active monoamine oxidase activity is obtained. Clorgyline and L-deprenyl are suicide enzyme inhibitors and irreversibly inhibit monoamine oxidase. When these inhibitors are labeled with carbon-11 they provide selective probes for monoamine oxidase localization and reactivity in vivo using positron emission tomography. 2 figs.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {Fri May 22 00:00:00 EDT 1987},
month = {Fri May 22 00:00:00 EDT 1987}
}